Identification of a potent kinase inhibitor targeting EML4-ALK fusion protein in non-small cell lung cancer

  • Medchemcomm. 2017 Aug 25;8(10):1914-1918. doi: 10.1039/c7md00305f.
Lian-Xiang Luo  1 ,  Ying Li  1 ,  Yu-Zhen Niu  2 ,  Yu-Wei Wang  1 ,  Qian-Qian Wang  1 ,  Xing-Xing Fan  1 ,  Jia-Hui Xu  1 ,  Liang Liu  1 ,  Elaine Lai-Han Leung  1 ,  Xiao-Jun Yao  1  2
Affiliations
  • 1. State Key Laboratory of Quality Research in Chinese Medicine/Macau Institute For Applied Research in Medicine and Health , Macau University of Science and Technology , Macau SAR , China . Email: [email protected] ; Email: [email protected] ; Email: [email protected] ; ; Tel: +853 8897 2409.
  • 2. State Key Laboratory of Applied Organic Chemistry and Department of Chemistry , Lanzhou University , Lanzhou 730000 , China.
PMID: 30108712 DOI: 10.1039/c7md00305f
Abstract

ALK-fusion proteins play a fundamental role in the development of about 5% of non-small cell lung cancers. Herein, we identified the compound 5067-0952 as a potent ALK inhibitor, which inhibited cell growth, induced Apoptosis, and suppressed the phosphorylation of ALK, subsequently blocking its downstream signaling pathway.